Novel AP2238-clorgiline hybrids as multi-target agents for the treatment of Alzheimer's disease: Design, synthesis, and biological evaluation

Guohui Zhong,Jie Guo,Chengyun Pang,Di Su,Chunli Tang,Lin Jing,Fengling Zhang,Ping He,Yaqian Yan,Zongji Chen,Jing Liu,Neng Jiang

Bioorganic Chemistry（2023）

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摘要

•A novel series of AP2238-clorgiline hybrids as anti-Alzheimer agents has been designed and synthesized.•5l showed the balanced and good inhibitory activity against AChE, BuChE and MAO-B.•5l exhibited no toxicity to PC12 and BV-2 cells at 12.5 μM and no acute toxicity at a dosage of 2500 mg/kg.•5l could significantly reverse scopolamine-induced memory deficit in mice and penetrate the BBB.

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关键词

Alzheimer’s disease,Clorgiline,Monoamine oxidase inhibitors,Cholinesterase inhibitors,Multi-target agents

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